Phosphodiesterase 5 (PDE5) is most familiar in connection to sildenafil (Viagra), a popular pharmaceutical PDE5 inhibitor. In response to nitric acid-activated soluble guanylyl cyclase production of cGMP, dimeric PDE5 binds and hydrolyzes cGMP in vascular smooth muscles cells, lung, kidney, brain, cardiac myocytes, and platelets to create 5′-GMP. This is accomplished by cGMP binding to […]
Researchers at the University of Tubingen use Transcreener to uncover how residence time works on a molecular level with p38α MAPK Inhibitors – Many factors affect the effectiveness of ligand-substrate or drug-target interactions. Conformational docking and stearic considerations help inform optimal “fits.” Ligand moiety solubility, both in free and bound forms, is also a consideration […]
OAS1 (Oligoadenylate synthetase 1) is induced by type 1 interferon signaling. It recognizes 18 bp (or longer) double stranded RNA segments from invading viruses in the cytosol and catalyzes the production of 2’-5’ linked oligoadenylate (2-5A) from ATP. The 2-5A then, at the expense of yet more ATP, exclusively activates endoribonclease L (RNase L) by […]
NUDT5 is found to be overexpressed in certain cancers in humans Could NUDT5 inhibitors lead to new cancer treatments? NUDIX hydrolases are a superfamily of enzymes are found in all classes of organisms and are responsible for hydrolyzing modified nucleoside diphosphates. One of the most well-studied NUDIX hydrolases is NUDT1 (also known as MTH1); it […]
Autoimmune disorders such as multiple sclerosis, psoriasis, and rheumatoid arthritis (RA), just to name a few, affect millions of people and have various contributing factors that lead to disease; some known and some unknown. These disorders occur due to the immune system’s failure to discriminate between self vs. foreign entities. Janus Kinase 3 (JAK3) is […]
Kinases are essential players in cellular functions such as cell signaling, cellular transport, and protein regulation. For these reasons, many kinases are innate immunity targets. A kinase assay kit is ideal whether used for drug screening and dose-response measurements or detection when studying a particular cellular pathway. A universal ADP assay allows researchers to screen […]
Cancer is complex, which makes determining the culprit as well as individual treatment extremely challenging. A variety of cancer types exist with a multitude of contributors. As the second leading cause of death in the US, cancer has been a target scientists have been battling for decades. When DNA is damaged or mutations occur, cells […]
Launched in November 2019, the Transcreener cGAMP cGAS Assay has generated a great deal of interest in the drug discovery community. While fluorescence polarization (FP) readouts offer a stable and robust option, some researchers prefer time-resolved Förster-resonance-energy-transfer (TR-FRET) readouts for large screens. After months of development, BellBrook Labs is pleased to announce the addition of […]
BellBrook Labs scientists have developed a new universal UDP detection assay for the measurement of Glycosyltransferase activity. The Transcreener UDP2 FI Assay extends the Transcreener platform for UDP detection by utilizing a simple fluorescence intensity (FI) output. It can be used on fluorescence readers typically found in academic and therapeutic research laboratories, as well as […]
The new Transcreener CD73 Assay measures adenosine production by CD73 in a mix-and-read format with a far-red fluorescence polarization readout. The assay will accelerate efforts to discover selective CD73 antagonists for cancer immunotherapy by enabling high throughput screening, structure-driven hit-to-lead, and mechanistic studies with the purified enzyme. Madison, WI – April 27th, 2020 – Researchers […]
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